Download Files:
ARN-21934
Price range: 90 CAD through 1,589 CAD
For Research Use Only (RUO). This product is sold strictly for laboratory research use. Not for human or veterinary consumption, therapeutic, or diagnostic use.For sale to research organizations and laboratories only; not for patients or for personal use.
Products Details
Product Description
– ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg/kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg/mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.
For Research Use Only (RUO). This product is sold strictly for laboratory research use only. Not for human or veterinary consumption, therapeutic, or diagnostic use. Any pharmacological, therapeutic, cosmetic, or biological effects described above are provided as research context only and do not represent intended or approved uses of this product.
Web ID
– T36968
Storage Temperature
– -20℃
Shipping
– Blue Ice
Molecular Formula
– C21H24N6
References
– Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.
CAS Number
– 2230854-93-8
Molecular Weight
– C21H24N6
Compound Purity
– 1
SMILES
– CN(C)c1ccc(Nc2nc(nc3CCC(N)Cc23)-c2ccncc2)cc1
Pathway
– DNA Damage/DNA Repair
Product type
– Small Compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
Related Products
1000 in stock
1000 in stock
Proudly representing
150+ years of combined research-supply heritage
